1. Field of the Invention
The present invention relates to a novel substance, the substance FKI-3864 which is useful for prevention and treatment of obesity and associated diseases through inhibition of the synthesis of intracellular triacylglycerols and a method of preparing the same. The present invention also relates to a novel microorganism capable of producing the substance FKI-3864 and a use of the substance FKI-3864.
2. Description of Related Art
Obesity is a condition in which excess neutral fat, mainly in the form of triacylglycerols, has accumulated in the adipose tissue due to excessive energy intake. In an obese subject, hypertrophy of the adipose tissue produces dysregulation of adipocytokines and as a result causes impaired glucose tolerance and hyperlipemia. Therefore, obesity is considered to be a significant risk factor of so-called lifestyle-related diseases such as hyperlipemia, diabetes, and hypertension.
Antiobestic drugs which are currently used include centrally-acting anorectic drugs such as mazindol (Novartispharma) which is a noradrenergic agent, sibutramine (Eisai) which is a serotonin noradrenarin reuptake inhibitor, and rimonabant (Sanofi-aventis) which is a cannabinoid receptor antagonist and a pancreatic lipase inhibitor such as orlistat (Chugai Pharmaceutical). Centrally-acting anorectic drugs cause appetite suppression, thereby leading to a reduction in lipid absorption, but they sometimes impair the health of a subject due to their anorectic activity and may produce side effects such as thirst, constipation, auditory hallucination, visual hallucination, and dependency. A pancreatic lipase inhibitor may cause side effects in the digestive tract such as diarrhea, incontinence, and steatorrhea. Accordingly, it is desired to develop a novel antiobestic drug having no side effects.
In view of the fact that excessive accumulation of triacylglycerols in the adipose tissue causes obesity, a substance which inhibits the biosynthesis of triacylglycerols is expected to exhibit an antiobestic activity having a mechanism which is different from that of existing drugs.
With respect to a substance inhibiting accumulation of triacylglycerols, it is reported that a substance having an inhibitory activity on a diacylglycerol acyltransferase is produced by a microorganism (Patent Documents 1, 2, and 3).    Patent Document 1: JP 08-182496 A1    Patent Document 2: WO 99/41265 A1    Patent Document 3: WO 00/58491 A1